CAS: 27757-85-3; 2-Thiophenemethylamine

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CAS号1003-31-2 2-氰基噻吩 | CAS号29683-84-9 噻酚-2-甲醛肟 | CAS号5813-89-8 2-噻吩甲酰胺 | CAS号45438-73-1 2-溴甲基噻吩 | CAS号98-03-3 2-噻吩甲醛 | CAS号636-72-6 2-噻吩甲醇 | CAS号188290-36-0 Thiophene(SIV) | CAS号50-00-0 甲醛 | CAS号57784-57-3 N-(thiophen-2-y... | CAS号26019-17-0 N,N-二甲基噻吩-2-甲胺,盐酸盐 | CAS号5813-89-8 2-噻吩甲酰胺 | CAS号58924-53-1 N-(2-噻吩甲基)-1-丁胺 | CAS号1003-31-2 2-氰基噻吩 | CAS号332082-90-3 5-[[bis(prop-2-... | CAS号347324-95-2 2-Cyano-N-(2-th... | CAS号30717-57-8 N,N-dimethylthi... | CAS号131436-78-7 4-羟基-5-氧代-1-(2-... | CAS号140-19-2 2-Pyridinamine,... | CAS号166964-34-7 5-(4-氯苯胺甲基)噻吩-2-磺酰氯

2-甲基-2-丙基(2-噻吩基甲基)氨基甲酸酯置于三氟乙酸体系中,用 二氯甲烷 用作溶剂,以81.5%的收率获得2-噻吩甲胺
参考文献:一些新型的噻吩类喹唑啉衍生物作为egfr抑制剂的合成及生物学评价
标题:一些新型的噻吩类喹唑啉衍生物作为egfr抑制剂的合成及生物学评价
摘要:背景:随着吉非替尼,厄洛替尼,阿法替尼和奥西替尼的临床批准,人们一直在大力追求靶向表皮生长因子受体(egfr)的药物.与大多数疗法类似,随着时间的推移,出现了与针对这些药物的治疗抗性相关的挑战,因此需要开发新的egfr酪氨酸激酶抑制剂(tki).本研究旨在研究一系列带有噻吩的喹唑啉衍生物作为egfr抑制剂的潜在用途.我们设计并合成了9种喹唑啉衍生物,其中首次报道了5种化合物(5E,5F,5G,5H和5I). 方法:用这些化合物处理两种癌细胞系,A431(过表达egfr)和a549(egfr野生型和kras突变),并进行mtt分析.选择a431细胞用于进一步处理(5E)和蛋白质印迹分析. 结果:尽管这些化合物对a549细胞的增殖没有明显的影响,但9种化合物中有7种显着抑制了a431细胞的生长.特别是5E和厄洛替尼的ic50值几乎相等.蛋白质印迹结果显示5E显着抑制a431细胞中的egfr自磷酸化.结构-活性关系表明,带有6
Doi:10.2174/1570180815666180803125935

专利信息

专利号:US-6228988-B1
优先权日:1995-02-24
标题:Synthesis of hydroxamic acid derivatives
发明人：FLOYD CHRISTOPHER DAVID; LEWIS CHRISTOPHER NORMAN
权利人:BRITISH BIOTECH PHARM
摘要:The present invention describes processes for preparing desired synthetic products that comprise a covalently bonded hydroxamic acid group -CONHOH by forming a mixture of a liquid reaction medium and a solid phase reaction product that carries a plurality of moieties of formula (A1) or (B1):where X is a residual, non-hydroxamate partial structure of the desired synthetic product, P1 is hydrogen or an amino-protecting group, P2 is hydrogen or a hydroxyl protecting group, and the bond designated (a) covalently links the moieties (A1) or (B1) to the residue of a solid substrate; by cleaving the bond designated (a) in the resultant mixture; and by separating the resultant liquid reaction phase from the resultant reaction solids to recover the desired synthetic product.

专利号:US-7157477-B2
优先权日:2000-10-25
标题 :Aliphatic amino-substituted demethoxylated hypocrellins and their synthesis
发明人：ZHANG MANHUA; XU SHANGJIE; WU TAO; CHEN SHEN; SHEN TAO
权利人:INST OF PHOTOGRAPHIC CHEMISTRY
摘要:The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.

专利号:US-5215997-A
优先权日:1985-09-11
标题:Synthesis of beta-lactam compounds
发明人：HUNGERBUEHLER ERNST; KALVODA JAROSLAV
权利人:CIBA GEIGY CORP
摘要:The invention relates to an improved process for the preparation of compounds of formula ##STR1## or salts thereof, starting from compounds of formulae ##STR2## via compounds of formulae ##STR3## in which compounds R 1 is hydrogen or lower alkyl, R 2 is an organic radical which may carry a functional group which may be protected by a customary protective group R 2 o , R 3 is hydrogen or a customary carboxyl protective group R 3 o , W is a group which can be replaced by a thiocarboxylic acid radical of formula III, and Z is oxygen or sulfur.

专利号:US-4388310-A
优先权日:1982-03-01
标 题:6-Amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids
发明人：CHRISTENSEN BURTON G; DININNO FRANK P; MUTHARD DAVID A; RATCLIFFE RONALD W
权利人:MERCK & CO INC
摘要:Disclosed are 6-amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids (I) which are useful as antibiotics and as intermediates in the synthesis of substituted pen-2-em-3-carboxylic acids: I wherein: R1 is H or acyl; R2 is hydrogen or methoxyl; R3 is alkyl having from 1-6 carbon atoms; phenylalkyl having 7-12 carbon atoms; and cycloalkyl having 3-6 carbon atoms; and R4 is hydrogen, a removable protecting group or a pharmaceutically acceptable salt or ester moiety.

专利号:US-4171439-A
优先权日:1975-04-11
标 题 :Antibacterial analogs of isocephalosporins
发明人：CONWAY TERRY T; LIM GARY M F; MENARD MARCEL
权利人:BRISTOL MYERS CO
摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein Z is halo or hydroxyl and X is acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.

专利号:US-9422321-B2
优先权日:2010-09-07
标题 :Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments
发明人：CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE
权利人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE; HIGH & NEW TECH RES CENTER HENAN ACAD OF SCIENCES; ZHENGZHOU GRANLEN PHARMATECH LTD; UNIV ZHENGZHOU
摘要:The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: n nAlso disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.